Self-emulsifying active substance formulation and use of this formulation
The present invention relates to self-emulsifying formulations based on an active ingredient component and a formulation base with a lipid component and with a binder component and to the use of this formulation as dosage form in the life science sector. The invention also describes a process for producing self-emulsifying formulations by mixing the formulation components to form a plastic mixture and, where appropriate, to manufacture the formulations as dosage form advantageously by use of melt extrusion. The formulations spontaneously form emulsions in water or aqueous media.
1. A solid, self-emulsifying formulation comprising
i) an active pharmaceutical ingredient
ii) 6 to 60% by weight of a lipid component, wherein the lipid component has an HLB of not exceeding 12 and has a melting point of not exceeding 40 ° C.; and
iii) 20 to 93.9% by weight of a binder component comprising a binder selected from polyvinylpyrrolidones, vinylpyrrolidone/vinylacetate copolymers, hydroxyalkylcelluloses, hydroxyalkylalkylcelluloses, cellulose phthalates or (meth)acrylic resins;
wherein the content of the lipid component based on the binder component does not exceed 40% by weight, and wherein the formulation is essentially free of lipid and active pharmaeutical ingredient crystals, and the formulation comprises a molecular dispersion of the lipid component in the binder component.
2. The formulation of claim 1 , wherein the active pharmaceutical ingredient has a low solubility in water.
3. The formulation of claim 1 , wherein the lipid component has a melting point of less than 30°C.
4. The formulation of claim 1 , wherein the lipid component is in the form of a molecular dispersion.
5. The formulation of claim 1 , wherein the content of the lipid component based on the binder component does not exceed 25% by weight.
6. The formulation of claim 1 , wherein the binder is selected from polyvinylpyrolidones, vinylpyrrolidone copolymers with vinyl acetate, hydroxypropylcelluloses or hydroxypropylmethylcelluloses.
7. The formulation of claim 1 , wherein the formulation is obtainable by melt extrusion of a plastic mixture comprising the components i), ii), and iii).
8. The formulation of claim 1 , wherein at least part of the active pharmaceutical ingredient is in the form of a molecular dispersion, and wherein the binder is selected from polyvinylpyrrolidones, vinylpyrrolidone copolymers with vinyl acetate, hydroxypropylcelluloses or hydroxypropylmethylcelluloses.
9. The formulation of claim 1 , wherein the formulation comprises 5 to 20% by weight of the active pharmaceutical ingredient.
10. The formulation of claim 9 , wherein the formulation comprises 30 to 90% by weight of the binder component.
11. The formulation of claim 1 , wherein the formulation is essentially amorphous.
12. The formulation of claim 11 , wherein the lipid component has an HLB of not exceeding 8.
13. The formulation of claim 11 , wherein the lipid component has an HLB of not exceeding 5.
14. The formulation of claim 11 , wherein the binder component is a vinylpyrrolidone/vinyl acetate copolymer having a vinylpyrolidone: vinyl acetate ratio of 60:40.
15. The formulation of claim 11 , wherein the formulation comprises 40 to 80% by weight of the binder component.
16. The formulation of claim 11 , wherein the binder component is selected from polyvinylpyrrolidone, vinylpyrrolidone copolymer with vinyl acetate, hydroxypropylcellulose, hydroxypropylmethylcellulose, hydroxypropylmethylcellulose phthalate, or a mixture thereof.
17. The formulation of claim 16 , wherein the formulation comprises 40 to 80% by weight of the binder component.
18. The formulation of claim 17 , wherein the active pharmaceutical ingredient has a low solubility in water.
19. The formulation of claim 18 , wherein the content of the lipid component based on the binder component does not exceed 25% by weight.
20. The formulation of claim 1 , wherein the formulation is capable of spontaneously forming an emulsion upon contact with aqueous media which contains at least 50% by weight water.
21. The formulation of claim 1 , wherein the lipid component is of liquid at room temperature.
22. The formulation of claim 1 , wherein the lipid component has an HLB of not exceeding 5.
23. The formulation of claim 20 , wherein the formulation is a tablet and comprises from 40 to 80% by weight of the binder component, and the content of the lipid component based on the binder component does not exceed 25% by weight.
24. The formulation of claim 11 , wherein the formulation is a tablet and comprises from 40 to 80% by weight of the binder component, and the content of the lipid component based on the binder component does not exceed 25% by weight.
25. The formulation of claim 24 , wherein the formulation is capable of spontaneously forming an emulsion upon contact with aqueous media contains at least 50% by weight water,and wherein the active pharmaceutical ingredient has low solubility in water.
26. The formulation of claim 25 , wherein the lipid component is of liquid at room temperature.
27. The formulation of claim 25 , wherein the lipid component has an HLB of not exceeding 5.
28. The formulation of claim 25 , wherein the binder component is polyvinylpyrrolidone, vinylpyrrolidone coploymer with vinyl acetate, hydroxypropylcellulose, hydroypropylmethylcellulose, hydroypropylmethylcellulose phthalate, or a mixture thereof.
29. The formulation of claim 25 , wherein the binder component is a vinylpyrrolidone/vinyl acetate copolymer with vinylpyrrolidone:vinyl acetate ratio of 60:40.